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Drug intelligence / Profile preview
PGA-PTX-E-[c(RGDfK)2]
- Development stage
- Preclinical
- Lead developer
- Centro de Investigación Príncipe Felipe
- Modality
- Small Molecules, Peptides, Biodegradable Polymers → Polymer-based Nanoparticles → Nanoparticles → Drug Delivery Systems
- Administration
- Intravenous
01
Overview
PGA-PTX-E-[c(RGDfK)2] is a nano-scaled polymer-drug conjugate designed for targeted cancer therapy and anti-angiogenesis. It consists of a biodegradable poly-L-glutamic acid (PGA) polymeric backbone conjugated to the cytotoxic chemotherapeutic agent paclitaxel (PTX) and a targeting moiety, the bis-cyclic RGD peptide E-[c(RGDfK)2]. The conjugate passively targets tumor tissues via the enhanced permeability and retention (EPR) effect, while the E-[c(RGDfK)2] peptide actively targets αvβ3 integrin, which is overexpressed on tumor endothelial cells and certain epithelial cancer cells. Once internalized into the lysosomal compartment of target cells, the PGA backbone is enzymatically degraded by cathepsin B, triggering the release of active paclitaxel. This dual-targeting approach enhances antitumor and anti-angiogenic efficacy while significantly reducing the systemic toxicities associated with free paclitaxel.
- Other names
- PGA-PTX-E-[c(RGD-fK)(2)]PGA-PTX-E-[c(RGDfK)]2poly(L-glutamic acid)-paclitaxel-E-[c(RGDfK)2]polyglutamic acid-paclitaxel-E-[c(RGDfK)2]polyglutamic acid-paclitaxel-E-[cyclo(Arg-Gly-Asp-D-Phe-Lys)]2
02
Targets
CTSB (Cathepsin B)αVβ3 (Integrin αVβ3)TUBB (Tubulin (alpha and beta subunits))
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